Neoandrographolide: A Comprehensive Encyclopedic Reference
1. Identity and Chemical Characterization
Chemical Names, CAS Number, and Formula
Neoandrographolide is a diterpenoid secondary metabolite derived from the plant Andrographis paniculata and is structurally a derivative of andrographolide. It is formally identified as the β-glucoside of ent-19-hydroxy-8(17),13-labdadien-16,15-olide. Among its systematic IUPAC names is {(1R,4aS,5R,8aS)-1,4a-dimethyl-6-methylene-5-[2-(2-oxo-2,5-dihydro-3-furanyl)ethyl]decahydro-1-naphthalenyl}methyl β-D-glucopyranoside, and it is also known by the alternate name neo-andrographolide.
Its molecular formula is C₂₆H₄₀O₈, with a molecular weight of 480.598 g/mol, and it is registered under CAS number 27215-14-1. This distinguishes it from its aglycone parent scaffold: the glucoside attachment (a β-D-glucopyranose unit) at C-19 is a defining structural feature that differentiates neoandrographolide from other diterpene lactones in the same plant.
Physical Properties
Neoandrographolide is a colorless column crystal isolated from the stem and leaves of Andrographis paniculata, with a melting point of 167–168 °C and a specific optical rotation of 48° (pyridine) and 45° (c = 1, absolute ethanol). It is soluble in methanol, ethanol, acetone, and pyridine, and slightly soluble in chloroform and water, but insoluble in ether and petroleum ether.
Botanical Source and Plant Parts
Neoandrographolide is isolated from the leaves of Andrographis paniculata. It has also been isolated from the stem of the same plant. Andrographis paniculata Nees belongs to the family Acanthaceae.
In the medicinal plant kalmegh (Andrographis paniculata), the C19-hydroxyl diterpene (andrograpanin) is predominantly found as C19-O-glucoside (neoandrographolide), whereas diterpenes having additional hydroxylation(s) at C3 (14-deoxy-11,12-didehydroandrographolide) or C3 and C14 (andrographolide) are primarily detected as aglycones, signifying scaffold-selective C19-O-glucosylation of diterpenes in the plant.
Isolation and Extraction
The dried leaves of A. paniculata are macerated in 95% ethanol and kept at room temperature for extraction. The residue is partitioned with ethyl acetate against water, and the ethyl acetate portion is chromatographed on a silica gel column, eluted with petroleum ether/acetone (7:3), yielding approximately 2 g of pure neoandrographolide (approximately 0.2% yield, w/w) from dried leaf material. The bioactive diterpenes andrographolide and neoandrographolide from the leaves of Andrographis paniculata have also been successfully separated by counter-current chromatography; a single 280-minute separation yielded 189 mg of 99.9% andrographolide and 9.5 mg of 98.5% neoandrographolide.
Relationship to Other Andrographis Constituents
The chemical constituents of Andrographis paniculata are mainly lactones and flavonoids, including the lactone compounds such as andrographolide and dehydrated andrographolide. In 1952, Kleipool first reported the separation of andrographolide from Andrographis paniculata. The leaves of A. paniculata contain several bioactive components, which include diterpene lactones (deoxyandrographolide, andrographolide, neoandrographolide, and 14-deoxy-11,12-didehydroandrographolide), diterpene glucosides, and flavonoids.
Neoandrographolide is listed in the Pharmacopoeia of the People's Republic of China (1977). Neoandrographolide and andrographolide are the main active ingredients of a variety of pharmaceutical preparations containing the Andrographis herb, such as andrographolide capsules, andrographolide tablets, Andrographis injection, potassium dehydroandrographolide succinate injection, Andrographis tablets, Xiaoyan Lidan tablets, and Fufang chuan xin lian tablets. These drugs are mainly used for treating acute bacterial dysentery, acute gastroenteritis, upper respiratory tract infection, acute tonsillitis, and pharyngitis, and are also used to treat malignant hydatidiform mole and choriocarcinoma.
2. Traditional and Historical Use
Overview of the Plant's Medicinal History
Neoandrographolide's traditional use is inseparable from that of its parent plant, Andrographis paniculata, as traditional healers used whole-plant preparations and did not isolate individual constituents. Andrographis paniculata, also called the "King of Bitterness" for its exceedingly bitter properties, belongs to the genus Andrographis and is a popular traditional medicinal plant widely distributed in Asian countries such as India, China, Malaysia, and Sri Lanka. In traditional Indian and Chinese medicine, it has been used for more than 1,000 years to treat inflammatory diseases.
Ayurvedic Tradition (India)
Andrographis paniculata, commonly known as "king of bitters," belongs to the Acanthaceae family and is native to South Asian countries, particularly India and Sri Lanka, where it is revered in traditional medicine systems such as Ayurveda. Known as Kalmegh in Ayurveda, the plant has been used as an alterative (supporting the routes of detoxification), stomachic (supporting digestion), and as an immune supporter.
Andrographis paniculata (family Acanthaceae) is one of the most popular medicinal plants used traditionally for the treatment of an array of diseases such as cancer, diabetes, high blood pressure, ulcer, leprosy, bronchitis, skin diseases, flatulence, colic, influenza, dysentery, dyspepsia, and malaria for centuries in Asia, America, and Africa. The combination of Andrographis paniculata (Kalmegha), Tinospora cordifolia (Guduchi), and Solanum nigrum (Kakmachi) was traditionally used in the Indian System of Medicine (Ayurveda) for the treatment of various liver-related disorders.
Traditional Chinese Medicine (TCM)
Andrographis paniculata plays a prominent part in Traditional Chinese Medicine, where it is known as "Chuan Xin Lian." It is frequently used in TCM to eliminate heat and toxins from the body, making it a popular choice for managing respiratory and immune system disorders. Its bitter character is consistent with the TCM theory of bitter herbs cleansing and detoxifying the body.
In the theory of traditional Chinese medicine, the medicinal property of A. paniculata belongs to 'cold', which exhibits the effect of clearing heat, detoxifying, cooling blood, and reducing swelling. A. paniculata has a long history of application in TCM theory, as well as in the traditional Indian medicine system Ayurveda. As a traditional Chinese medicine, Chuanxinlian has been used clinically in the treatment of respiratory tract infections, acute dysentery, gastroenteritis, fever and flu, hypertension, and other diseases.
Traditional Preparations
The plant Andrographis paniculata has been extensively used in traditional medicine as a bitter tonic, febrifuge, and in bowel complaints. Traditional herbal treatment applications have included diarrhea, dysentery, cholera, pneumonia, swollen lymph nodes, leprosy, bronchitis, sore throats, tuberculosis, chicken pox, coughs, headaches, ear infection, inflammation, burns, and mumps.
Typical traditional preparations consisted of decoctions, powdered leaf, and whole-plant extracts. The active ingredients in Chuanxinlian are reported to include andrographolide lactones, among them andrographolide (AND), neoandrographolide (NAND), 14-deoxy-andrographolide (DAND), and 14-deoxy-11,12-dehydroandrographolide (DDAND).
3. Key Constituents, Phytochemistry, and Biosynthesis
Chemical Classification
Neoandrographolide is classified as a diterpenoid secondary metabolite belonging more specifically to the ent-labdane class of diterpenoids. The labdane diterpenes represent a large class of phytochemicals with many pharmacological benefits, such as anti-inflammatory, hepatoprotective, and anticarcinogenic properties.
Biosynthesis Within the Plant
In Andrographis paniculata, UDP-glycosyltransferase (UGT) activity shows an apparent correlation with the spatio-temporal accumulation of neoandrographolide as the major C19-O-glucoside diterpene of the plant. Nitrogen sources remarkably affect the content of diterpenoid lactone components, including neoandrographolide, along with carbon and nitrogen metabolism reprogramming in Andrographis paniculata.
Coexisting Active Compounds
Andrographis paniculata contains four major active diterpenoids, including andrographolide (1), 14-deoxy-11,12-didehydroandrographolide (2), neoandrographolide (3), and 14-deoxyandrographolide (4), which exhibit differences in types and/or degrees of their pharmacological activity.
4. Established Mechanisms of Action
Anti-Inflammatory Mechanisms
Neoandrographolide exhibits anti-inflammatory activities by affecting cyclooxygenase (COX)-1 and -2, and by down-regulating the expression of genes associated with the inflammation response, including cytokines and cytokine receptors, chemokines, JAK/STAT signaling, TLR family members, and NF-κB.
Neoandrographolide inhibits COX-2 protein expression without inhibiting COX-2 mRNA expression, which contributes to its inhibitory activity against PGEâ‚‚ overproduction. This suggests that the effect of neoandrographolide on iNOS expression may occur at the transcriptional level, while the inhibition of COX-2 expression occurs at the translational level. Furthermore, neoandrographolide has been shown to inhibit the activation of p38 mitogen-activated protein kinase (MAPK).
Neoandrographolide can inhibit lipopolysaccharide-induced nitric oxide (NO) production in mouse peritoneal macrophages and inhibits the release of endothelin and malondialdehyde induced by oxidized low-density lipoprotein (ox-LDL) in porcine aortic cells.
Cardiovascular and Lipid-Modulating Mechanisms
Plasma aspartate transaminase and alanine transaminase levels were significantly decreased by feeding with andrographolide and neoandrographolide in rats compared with the positive group (simvastatin). Andrographolide and neoandrographolide protect the cardiovascular system through down-regulation of iNOS expression and up-regulation of eNOS expression.
Neoandrographolide inhibits iNOS and the generation of reactive oxygen species (ROS), and activates eNOS, exhibiting anti-inflammatory and hypolipidemic activity.
Anticancer Mechanisms
Using a series of in silico and cell experimental validations, neoandrographolide (NAP) has been demonstrated to be a novel Rab5 inhibitor that occupies the GTPase groove to limit Rab5 activation, resulting in the subsequent blockage of EGFR degradation and ERK signaling-mediated cell proliferation. Rab5 is a small GTPase that plays a crucial role in oncogenic signal transduction and was considered an attractive target for cancer therapy; rapid GDP/GTP exchange in the packet of Rab5 sustains its high activity for promoting cancer progression.
Western blot findings indicate that neoandrographolide inhibits the phosphorylation of ERK, P38, JNK, and P65 but does not reverse the degradation of IκB-α. Additionally, neoandrographolide affects the phosphorylation of proteins in the PI3K/AKT, GSK3β, and PPARγ pathways.
Immunostimulant Mechanisms
In 1993, Puri et al. revealed the in vivo immunostimulant activity of A. paniculata ethanolic extract and the purified diterpenes andrographolide and neoandrographolide. The stimulation of both antigen-specific and nonspecific immune responses was observed, resulting in the enhancement of humoral and cell-mediated immune responses to sheep red blood cells (SRBC), as well as the macrophage migration index (MMI) phagocytosis and the proliferation of splenic lymphocytes in treated mice.
Osteoclast Modulation
Neoandrographolide inhibits osteoclast differentiation and bone resorption through inhibition of the MAPK/NF-κB/PI3K/AKT/GSK3β/PPAR/CAMK signaling pathway.
Cardioprotective Mechanism
Neoandrographolide inhibits apoptosis in rat embryonic ventricular cardiomyocytes, suggesting a potential cardioprotective mechanism at the cellular level.
5. Scientific Evidence by Area of Use
5.1 Anti-Inflammatory Activity
Preclinical (in vitro and animal) evidence: Neoandrographolide, one of the principal diterpene lactones isolated from Andrographis paniculata, has been tested in vivo and in vitro for its anti-inflammatory activities and mechanism. Oral administration of neoandrographolide at 150 mg/kg significantly suppressed ear edema induced by dimethyl benzene in mice. Oral administration of neoandrographolide at 150 mg/kg significantly suppressed ear edema induced by dimethyl benzene in mice, and oral administration at 100–150 mg/kg also reduced the increase in vascular permeability induced by acetic acid in mice.
A study investigated the anti-aging effects of methanolic extract, andrographolide, neoandrographolide, 14-deoxyandrographolide, and 14-deoxy-11,12-didehydroandrographolide on human dermal fibroblasts under pro-oxidant or pro-inflammatory conditions. The in vitro anti-aging capacity was tested at concentrations of 1, 2.5, and 5 µg/mL in human dermal fibroblasts (HDFa).
Evidence strength: Anti-inflammatory evidence for neoandrographolide as an isolated compound is primarily preclinical (in vitro and rodent models). No published human clinical trials have specifically examined neoandrographolide as an isolated compound for inflammatory endpoints. The mechanistic data is detailed and internally consistent but requires translation to human clinical studies before conclusions about efficacy in humans can be drawn.
5.2 Lipid-Lowering (Hypolipidemic) Activity
Animal evidence: Andrographolide (AND) and neoandrographolide (NEO) are diterpenoids from Andrographis paniculata (Acanthaceae). A study investigated the hypolipidemic effect of AND and NEO in hyperlipidemic mice induced by 75% yolk emulsion and in hyperlipidemic rats induced by high-fat emulsion. The results showed that the levels of triglyceride, total cholesterol, and low-density lipoprotein cholesterol were reduced by AND and NEO in a dose-dependent tendency in mice. Compared with the model group, the plasma total cholesterol levels of experimental groups with AND and NEO at 100 mg/kg dosage decreased by 23.9% and 20.2% in rats, respectively (P < 0.05).
In conclusion, andrographolide and neoandrographolide have potent hypolipidemic effects and protect the cardiovascular system without significant liver damage.
Evidence strength: This evidence is animal-model only (mice and rats). The specific dose of 100 mg/kg for rodents does not directly translate to a human-equivalent dose without further pharmacokinetic data. No human randomized controlled trials have examined neoandrographolide specifically for lipid lowering.
5.3 Anticancer and Chemosensitizing Activity
In vitro and computational evidence: Rab5 was considered an attractive anticancer target but remained undruggable due to the lack of a specific inhibitor. Neoandrographolide (NAP) was reported as a novel Rab5 inhibitor, discovered by high-throughput virtual screening with a natural product library containing 7,459 compounds; it can occupy the surface groove of Rab5, competing with GDP/GTP for binding.
Neoandrographolide (NAP), a compound isolated from Andrographis paniculata, was identified with a higher docking score and good ADMET prediction. Using a series of in silico and cell experimental validations, NAP was demonstrated to be a novel Rab5 inhibitor, resulting in the subsequent blockage of EGFR degradation and ERK signaling-mediated cell proliferation. NAP may be further explored as an anti-tumor drug targeting Rab5 for clinical cancer therapy.
Neoandrographolide has also been studied as a chemosensitizer in S-Jurkat and X chromosome-linked inhibitor of apoptosis protein (XIAP)-overexpressing Jurkat cells, a model for chemoresistance.
Evidence strength: Anticancer evidence for neoandrographolide as an isolated compound is entirely preclinical (computational docking, cell line studies). No human or animal in vivo tumor studies have been published specifically for isolated neoandrographolide in this context. This must be characterized as very preliminary.
5.4 Immunomodulatory Activity
In 1993, Puri et al. revealed the in vivo immunostimulant activity of A. paniculata ethanolic extract and the purified diterpenes andrographolide and neoandrographolide. The stimulation of both antigen-specific and nonspecific immune responses was observed, resulting in the enhancement of humoral and cell-mediated immune responses to sheep red blood cells (SRBC), as well as the macrophage migration index (MMI) phagocytosis and the proliferation of splenic lymphocytes in treated mice.
Evidence strength: Immunostimulant data for neoandrographolide is largely from animal (in vivo rodent) experiments. The clinical immunological effects of neoandrographolide as an isolated compound in humans have not been assessed in published controlled trials.
5.5 Antiviral and Anti-Infective Activity
Neoandrographolide has broad pharmacological activities, including anti-inflammatory, anti-HIV, anti-cancer, antihepatitis, anti-infective, and hepatoprotective properties. Neoandrographolide is known for its antiviral, anticancer, hepatoprotective, antioxidant, and anti-inflammatory properties.
Human clinical data for antiviral activity specifically attributed to neoandrographolide as an isolated compound is limited. The clinical evidence that exists relates primarily to whole-plant Andrographis paniculata extracts or andrographolide derivatives — not to neoandrographolide in isolation. Clinical studies have been conducted to investigate the efficacy of A. paniculata in the treatment of viral infectious diseases, including influenza, herpes simplex virus (HSV), human immunodeficiency virus (HIV), coronavirus (SARS-CoV-2), and upper respiratory tract infections (URTIs).
Evidence strength: In the context of COVID-19 studies, neoandrographolide has been measured as one of the four major pharmacokinetically tracked diterpenoids, but clinical efficacy has been studied for the total extract rather than for neoandrographolide specifically.
5.6 Hepatoprotective Activity
Neoandrographolide is consistently cited among the hepatoprotective constituents of Andrographis paniculata. A. paniculata is widely used traditionally as a hepatoprotective agent and a stimulating agent for multiple enzymes of the liver. Dealkenylated neoandrographolide (DN) has exhibited hepatoprotective, cholesterol synthesis and absorption inhibition property, and β-glucuronidase inhibition activity.
Plasma aspartate transaminase and alanine transaminase levels were significantly decreased by administration of andrographolide and neoandrographolide in rats compared with the simvastatin-treated positive group (P < 0.01), suggesting hepatoprotective effects at the lipid-lowering doses studied.
Evidence strength: Hepatoprotective evidence is animal-based. No human randomized controlled trials have evaluated isolated neoandrographolide specifically for liver protection.
5.7 Cardiovascular Protection
Andrographolide and neoandrographolide protect the cardiovascular system through down-regulation of iNOS expression and up-regulation of eNOS expression, and have potent hypolipidemic effects without causing significant liver damage.
Neoandrographolide inhibits the release of endothelin and malondialdehyde induced by oxidized low-density lipoprotein (ox-LDL) in porcine aortic cells, suggesting a mechanism of vascular protection against oxidative lipid injury.
Evidence strength: Entirely preclinical (animal and ex vivo cell models). No dedicated human cardiovascular trials exist for isolated neoandrographolide.
5.8 Antioxidant Activity
Neoandrographolide is known to have hypolipidemic, anti-inflammatory, and anti-oxidant effects, and protects the cardiovascular system without significant liver damage. Its antioxidant properties have been characterized in both in vitro radical-scavenging assays and ex vivo models involving ROS production. Neoandrographolide inhibits iNOS and the generation of ROS, contributing to its anti-inflammatory and hypolipidemic profile.
Evidence strength: In vitro and animal-based; no human clinical trial data exist specifically for neoandrographolide's antioxidant effects.
5.9 Anti-Fever Activity
A study by Deng discovered that andrographolide, neoandrographolide, and dehydroandrographolide were active constituents in relieving fever in preclinical models.
Evidence strength: Preclinical only. Human data on antipyretic properties of neoandrographolide specifically are not available in the published literature reviewed.
6. Body Systems and Health Areas of Association
- Immune System: Immunostimulation, enhancement of humoral and cell-mediated immune responses, macrophage activation, lymphocyte proliferation.
- Inflammatory Pathways: Inhibition of NF-κB, p38 MAPK, iNOS, COX-2, and prostaglandin E₂ production; reduction of proinflammatory cytokines.
- Cardiovascular System: Lipid lowering, endothelial protection via eNOS upregulation and iNOS downregulation, ox-LDL-induced vascular injury mitigation.
- Hepatic System: Hepatoprotection, normalization of liver enzyme markers (AST, ALT), and protection from drug- and toxin-induced liver injury.
- Oncology (preclinical): Antiproliferative actions via Rab5/EGFR/ERK pathway inhibition; chemosensitization in leukemia models; multi-pathway modulation (PI3K/AKT, MAPK).
- Respiratory System: Part of the phytochemical basis for the traditional and clinical use of A. paniculata in upper respiratory tract infections.
- Musculoskeletal System: Inhibition of osteoclast differentiation and bone resorption via MAPK/NF-κB/PI3K pathway suppression.
- Antiviral Defense: Included within the active constituents of the plant studied against HIV, hepatitis, and SARS-CoV-2.
7. Pharmacokinetics
Clinical pharmacokinetic studies have tracked neoandrographolide alongside the other major active diterpenoids — andrographolide, 14-deoxy-11,12-didehydroandrographolide, and 14-deoxyandrographolide — after oral administration of Andrographis paniculata aqueous extract in human subjects.
Results indicated a dose-dependent effect between two extract doses. A twofold increase in the dose of the extract demonstrated twofold higher plasma concentrations of the four major parent compounds (andrographolide, 14-deoxy-11,12-didehydroandrographolide, neoandrographolide, and 14-deoxyandrographolide), as well as their conjugated metabolites. The observed diterpenoids are biotransformed partly through a phase II metabolic pathway of conjugation, thereby reducing the concentration of parent compounds in the plasma, with the majority existing as conjugated metabolites.
Mean plasma concentration-time profiles of neoandrographolide were tracked after single (30 mg of andrographolide equivalent) and multiple (90 mg/day of andrographolide) oral administration of standardized A. paniculata aqueous extract capsules for 5 consecutive days in patients with mild COVID-19, with data presented as mean ± SD (n = 12).
The four major diterpenoids exhibited rapid absorption and elimination with limited systemic exposure, supporting repeated dosing to maintain adequate exposure over the 5-day dosing period.
8. Dosage Forms and Reported Dosages
No standardized clinical dosage for isolated neoandrographolide has been established. Reported dosages from preclinical and clinical studies (which used whole extract or andrographolide-equivalent quantification) include the following:
- Rodent anti-inflammatory (in vivo): Oral administration of neoandrographolide at 150 mg/kg significantly suppressed ear edema induced by dimethyl benzene in mice.
- Rodent vascular permeability model (in vivo): Oral administration of neoandrographolide at 100–150 mg/kg reduced the increase in vascular permeability induced by acetic acid in mice.
- Rodent hypolipidemic model (in vivo): AND and NEO at 100 mg/kg dosage in rats reduced plasma total cholesterol levels by 23.9% and 20.2%, respectively (P < 0.05).
- In vitro (human dermal fibroblasts): Neoandrographolide was tested at concentrations of 1, 2.5, and 5 µg/mL.
- Human pharmacokinetic study (standardized extract): Aqueous extract capsules were orally administered at 60 or 120 mg, three times a day (equivalent to 180 or 360 mg/day of andrographolide) for 7 consecutive days in healthy participants.
- Human clinical (COVID-19 patients): Standardized A. paniculata aqueous extract capsules were administered as a single dose (30 mg of andrographolide equivalent) and multiple doses (90 mg/day of andrographolide) for 5 consecutive days.
Neoandrographolide is available as a pure isolated reference standard (purity 95–99%) for research purposes and appears as a constituent in standardized Andrographis paniculata herbal preparations. It is not typically marketed or sold as a single-compound dietary supplement in isolation.
9. Safety Considerations and Known Interactions
General Safety Profile from Clinical Studies (Whole-Plant Preparations)
Andrographolide derivative medications and herbal preparations of Andrographis paniculata are often used to treat respiratory tract infections. A systematic review and meta-analysis aimed to systematically evaluate the safety of these preparations based on clinical studies.
A total of 262 studies were included in that review, including 125 randomized controlled trials, 23 non-randomized controlled trials, 6 case series, and 108 case reports. In 9,490 participants using andrographolide derivative injections, 383 (4.04%) reported adverse drug reactions. Meta-analysis showed that the adverse drug reaction incidence of the three most frequently used andrographolide derivative injections (andrographolide sulfonate, potassium sodium dehydroandrographolide succinate, and potassium dehydroandrographolide succinate) were 5.48%, 3.69%, and 5.33%, respectively.
Adverse Events in Clinical Pharmacokinetic Studies
The dosing regimen of 90 mg of andrographolide per day (from standardized whole extract in which neoandrographolide was a tracked constituent) was well tolerated, with only mild adverse events reported and no evidence of hepatotoxicity or renal toxicity.
Available information on the safety of the aqueous extract specifically at high doses remains limited.
Adverse Events Noted for Andrographolide-Containing Products
Adverse reactions (including headache, fatigue, rash, bitter/metallic taste, diarrhea, pruritus, and decreased sex drive) during a phase 1 study of andrographolide in patients who were HIV positive and healthy volunteers required interruption of the study. These events were attributed specifically to a purified andrographolide formulation at higher doses rather than to standard herbal preparations.
Hepatotoxicity Considerations
In the animal hypolipidemic study, andrographolide and neoandrographolide demonstrated potent hypolipidemic effects and protected the cardiovascular system without causing significant liver damage. Furthermore, in the pharmacokinetic clinical study, no hepatotoxicity or renal toxicity was observed at the doses studied in patients with mild COVID-19.
Interaction Potential
No published clinical interaction studies exist specifically for isolated neoandrographolide. The broader literature on Andrographis paniculata preparations notes a theoretical potential for interactions with immunosuppressant medications, anticoagulants, and antihypertensive agents given the plant's demonstrated immunostimulant, platelet-modulating, and blood pressure-related activities. AP has the pharmacological effects of anti-inflammatory, antibacterial, antiviral, antihyperglycemic, anticancer, antistress, hepatoprotective, and immunomodulatory activities. Herbal preparations of AP have been used to treat respiratory tract infections, colitis, early stages of COVID-19, and to relieve the symptoms of arthritis. The pharmacological breadth of the plant's constituent profile suggests potential for additive or antagonistic effects with drugs operating on overlapping pathways, but specific interaction data for neoandrographolide in isolation is not available in the published clinical literature.
Pharmacopoeial Recognition
Neoandrographolide is available in the Pharmacopoeia of the People's Republic of China (1977), reflecting its long-standing official recognition in Chinese herbal medicine regulatory standards.
10. Summary of Evidence Strength
The body of published scientific evidence for neoandrographolide can be characterized as follows:
- Mechanism of action (in vitro): Well-characterized across multiple pathways (NF-κB, p38 MAPK, iNOS/COX-2, Rab5/EGFR, PI3K/AKT). Evidence quality is high at this level.
- Animal in vivo pharmacology: Demonstrated for anti-inflammatory, hypolipidemic, immunostimulant, and cardiovascular protective effects. Data are consistent but use rodent models with doses in the range of 100–150 mg/kg.
- Human clinical evidence for neoandrographolide specifically: Absent as an isolated compound. Clinical pharmacokinetic profiling confirms its presence and dose-proportional systemic exposure in humans when taking standardized A. paniculata extracts, but clinical efficacy endpoints have not been tested for neoandrographolide in isolation.
- Clinical evidence for the parent plant (A. paniculata) in which neoandrographolide is a key constituent: More robust, including randomized controlled trials for upper respiratory tract infections and COVID-19 symptom management, but these cannot be attributed specifically to neoandrographolide.
References
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